Home Hippo MAP4K inhibitor PF-6260933 For research use only.

PF-6260933

Synonyms: PF-06260933

PF-6260933 (PF-06260933) is a potent inhibitor of MAP4K4 with an IC50 of 3.7 nM, possessing excellent kinome selectivity.

PF-6260933 Chemical Structure

PF-6260933 Chemical Structure

CAS No. 1811510-56-1

Purity & Quality Control

PF-6260933 Related Products

Biological Activity

Description PF-6260933 (PF-06260933) is a potent inhibitor of MAP4K4 with an IC50 of 3.7 nM, possessing excellent kinome selectivity.
Targets
MAP4K4 [1]
3.7 nM
In vitro
In vitro

PF-6260933 demonstrates good physicochemical properties as well as moderate human liver microsomal (HLM) clearance[1].
In Vivo
In vivo

Following oral dosing (10 mg/kg), PF-6260933 displays a plasma exposure that provided free drug concentrations above the cell IC50 value for about 4-6 h after administration in a mouse model. PF-6260933 has suitable PK properties in mouse to be used as a tool in an in vivo model of diabetes[1].

Chemical Information & Solubility

Molecular Weight 296.75 Formula

C16H13ClN4
CAS No. 1811510-56-1 SDF --
Smiles C1=CC(=CC=C1C2=C(N=CC(=C2)C3=CN=C(C=C3)N)N)Cl
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 59 mg/mL ( (198.82 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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